Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase–Glucokinase Regulatory Protein (GK–GKRP) Binding: Strategic Use of a N → S (nN → σS–X) Interaction for Conformational Constraint
Pennington, Lewis D, Bartberger, Michael D, Croghan, Michael D, Andrews, Kristin L, Ashton, Kate S, Bourbeau, Matthew P, Chen, Jie, Chmait, Samer, Cupples, Rod, Fotsch, Christopher, Helmering, Joan, Hong, Fang-Tsao, Hungate, Randall W, Jordan, Steven R, Kong, Ke, Liu, Longbin, Michelsen, Klaus, Moyer, Carolyn, Nishimura, Nobuko, Norman, Mark H, Reichelt, Andreas, Siegmund, Aaron C, Sivits, Glenn, Tadesse, Seifu, Tegley, Christopher M, Van, Gwyneth, Yang, Kevin C, Yao, Guomin, Zhang, Jiandong, Lloyd, David J, Hale, Clarence, St. Jean, David J
Published in Journal of medicinal chemistry (24.12.2015)
Published in Journal of medicinal chemistry (24.12.2015)
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Discovery of Clinical Candidate 1‑(4-(3-(4-(1H‑Benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), A Potent, Selective, and Efficacious Inhibitor of Phosphodiesterase 10A (PDE10A)
Hu, Essa, Chen, Ning, Bourbeau, Matthew P, Harrington, Paul E, Biswas, Kaustav, Kunz, Roxanne K, Andrews, Kristin L, Chmait, Samer, Zhao, Xiaoning, Davis, Carl, Ma, Ji, Shi, Jianxia, Lester-Zeiner, Dianna, Danao, Jean, Able, Jessica, Cueva, Madelyn, Talreja, Santosh, Kornecook, Thomas, Chen, Hang, Porter, Amy, Hungate, Randall, Treanor, James, Allen, Jennifer R
Published in Journal of medicinal chemistry (14.08.2014)
Published in Journal of medicinal chemistry (14.08.2014)
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Discovery of a Potent, Orally Active 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitor for Clinical Study: Identification of (S)-2-((1S,2S,4R)-Bicyclo[2.2.1]heptan-2-ylamino)-5-isopropyl-5-methylthiazol-4(5H)-one (AMG 221)
Véniant, Murielle M, Hale, Clarence, Hungate, Randall W, Gahm, Kyung, Emery, Maurice G, Jona, Janan, Joseph, Smriti, Adams, Jeffrey, Hague, Andrew, Moniz, George, Zhang, Jiandong, Bartberger, Michael D, Li, Vivian, Syed, Rashid, Jordan, Steven, Komorowski, Renée, Chen, Michelle M, Cupples, Rod, Kim, Ki Won, St. Jean, David J, Johansson, Lars, Henriksson, Martin A, Williams, Meredith, Vallgårda, Jerk, Fotsch, Christopher, Wang, Minghan
Published in Journal of medicinal chemistry (10.06.2010)
Published in Journal of medicinal chemistry (10.06.2010)
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2-(S)-Phenethylaminothiazolones as Potent, Orally Efficacious Inhibitors of 11β-Hydroxysteriod Dehydrogenase Type 1
St. Jean, David J, Yuan, Chester, Bercot, Eric A, Cupples, Rod, Chen, Michelle, Fretland, Jenne, Hale, Clarence, Hungate, Randall W, Komorowski, Renee, Veniant, Murielle, Wang, Minghan, Zhang, Xiping, Fotsch, Christopher
Published in Journal of medicinal chemistry (08.02.2007)
Published in Journal of medicinal chemistry (08.02.2007)
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Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists
Chen, Jian Jeffrey, Qian, Wenyuan, Biswas, Kaustav, Viswanadhan, Vellarkad N., Askew, Benny C., Hitchcock, Stephen, Hungate, Randall W., Arik, Leyla, Johnson, Eileen
Published in Bioorganic & medicinal chemistry (15.08.2008)
Published in Bioorganic & medicinal chemistry (15.08.2008)
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Discovery of Novel, Potent Benzamide Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 (11β-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model
Julian, Lisa D, Wang, Zhulun, Bostick, Tracy, Caille, Seb, Choi, Rebekah, DeGraffenreid, Michael, Di, Yongmei, He, Xiao, Hungate, Randall W, Jaen, Juan C, Liu, Jinsong, Monshouwer, Mario, McMinn, Dustin, Rew, Yosup, Sudom, Athena, Sun, Daqing, Tu, Hua, Ursu, Stefania, Walker, Nigel, Yan, Xuelei, Ye, Qiuping, Powers, Jay P
Published in Journal of medicinal chemistry (10.07.2008)
Published in Journal of medicinal chemistry (10.07.2008)
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The discovery of 2-anilinothiazolones as 11β-HSD1 inhibitors
Yuan, Chester, St. Jean, David J., Liu, Qingyian, Cai, Lynn, Li, Aiwen, Han, Nianhe, Moniz, George, Askew, Ben, Hungate, Randall W., Johansson, Lars, Tedenborg, Lars, Pyring, David, Williams, Meredith, Hale, Clarence, Chen, Michelle, Cupples, Rod, Zhang, Jiandong, Jordan, Steven, Bartberger, Michael D., Sun, Yaxiong, Emery, Maurice, Wang, Minghan, Fotsch, Christopher
Published in Bioorganic & medicinal chemistry (15.11.2007)
Published in Bioorganic & medicinal chemistry (15.11.2007)
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Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5- a]pyrimidines: A New Class of KDR Kinase Inhibitors
Fraley, Mark E., Hoffman, William F., Rubino, Robert S., Hungate, Randall W., Tebben, Andrew J., Rutledge, Ruth Z., McFall, Rosemary C., Huckle, William R., Kendall, Richard L., Coll, Kathleen E., Thomas, Kenneth A.
Published in Bioorganic & medicinal chemistry letters (07.10.2002)
Published in Bioorganic & medicinal chemistry letters (07.10.2002)
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Discovery of Aryl Aminoquinazoline Pyridones as Potent, Selective, and Orally Efficacious Inhibitors of Receptor Tyrosine Kinase c-Kit
Hu, Essa, Tasker, Andrew, White, Ryan D, Kunz, Roxanne K, Human, Jason, Chen, Ning, Bürli, Roland, Hungate, Randall, Novak, Perry, Itano, Andrea, Zhang, Xuxia, Yu, Violeta, Nguyen, Yen, Tudor, Yanyan, Plant, Matthew, Flynn, Shaun, Xu, Yang, Meagher, Kristin L, Whittington, Douglas A, Ng, Gordon Y
Published in Journal of medicinal chemistry (12.06.2008)
Published in Journal of medicinal chemistry (12.06.2008)
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Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors: SAR, synthesis, and modeling evaluation
Tegley, Christopher M., Viswanadhan, Vellarkad N., Biswas, Kaustav, Frohn, Michael J., Peterkin, Tanya A.N., Chang, Catherine, Bürli, Roland W., Dao, Jennifer H., Veith, Henrike, Rogers, Norma, Yoder, Sean C., Biddlecome, Gloria, Tagari, Philip, Allen, Jennifer R., Hungate, Randall W.
Published in Bioorganic & medicinal chemistry (15.07.2008)
Published in Bioorganic & medicinal chemistry (15.07.2008)
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Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors
Rew, Yosup, McMinn, Dustin L., Wang, Zhulun, He, Xiao, Hungate, Randall W., Jaen, Juan C., Sudom, Athena, Sun, Daqing, Tu, Hua, Ursu, Stefania, Villemure, Elisia, Walker, Nigel P.C., Yan, Xuelei, Ye, Qiuping, Powers, Jay P.
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
Published in Bioorganic & medicinal chemistry letters (15.03.2009)
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2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics
Zeng, Qingping, Bourbeau, Matthew P., Wohlhieter, G. Erich, Yao, Guomin, Monenschein, Holger, Rider, James T., Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie, Freeman, Daniel, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey, Tasker, Andrew S., Dominguez, Celia, Viswanadhan, Vellarkad N., Hungate, Randall, Zhang, Xiaoling
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Discovery of dehydro-oxopiperazine acetamides as novel bradykinin B1 receptor antagonists with enhanced in vitro potency
Qian, Wenyuan, Chen, Jian Jeffrey, Human, Jason, Aya, Toshihiro, Zhu, Jiawang, Biswas, Kaustav, Peterkin, Tanya, Hungate, Randall W., Arik, Leyla, Johnson, Eileen, Kumar, Gondi, Joseph, Smriti, Jona, Janan, Guo, Hong-Xun, Wu, Zufan
Published in Bioorganic & medicinal chemistry letters (15.01.2012)
Published in Bioorganic & medicinal chemistry letters (15.01.2012)
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New ‘chemical probes’ to examine the role of the hFPRL1 (or ALXR) receptor in inflammation
Frohn, Mike, Xu, Han, Zou, Xiaoming, Chang, Catherine, McElvaine, Michele, Plant, Matthew H., Wong, Min, Tagari, Philip, Hungate, Randall, Bürli, Roland W.
Published in Bioorganic & medicinal chemistry (01.12.2007)
Published in Bioorganic & medicinal chemistry (01.12.2007)
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Further Studies with the 2-Amino-1,3-thiazol-4(5H)-one Class of 11β-Hydroxysteroid Dehydrogenase Type 1 Inhibitors: Reducing Pregnane X Receptor Activity and Exploring Activity in a Monkey Pharmacodynamic Model
Fotsch, Christopher, Bartberger, Michael D, Bercot, Eric A, Chen, Michelle, Cupples, Rod, Emery, Maury, Fretland, Jenne, Guram, Anil, Hale, Clarence, Han, Nianhe, Hickman, Dean, Hungate, Randall W, Hayashi, Michael, Komorowski, Renee, Liu, Qingyian, Matsumoto, Guy, St. Jean, David J, Ursu, Stefania, Véniant, Murielle, Xu, Guifen, Ye, Qiuping, Yuan, Chester, Zhang, Jiandong, Zhang, Xiping, Tu, Hua, Wang, Minghan
Published in Journal of medicinal chemistry (25.12.2008)
Published in Journal of medicinal chemistry (25.12.2008)
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Effect of microwave heating on Ullmann-type heterocycle-aryl ether synthesis using chloro-heterocycles
D’Angelo, Noel D., Peterson, Joseph J., Booker, Shon K., Fellows, Ingrid, Dominguez, Celia, Hungate, Randall, Reider, Paul J., Kim, Tae-Seong
Published in Tetrahedron letters (17.07.2006)
Published in Tetrahedron letters (17.07.2006)
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3-Oxo-2-piperazinyl acetamides as potent bradykinin B1 receptor antagonists for the treatment of pain and inflammation
Chen, Jian Jeffrey, Nguyen, Thomas, D’Amico, Derin C., Qian, Wenyuan, Human, Jason, Aya, Toshihiro, Biswas, Kaustav, Fotsch, Christopher, Han, Nianhe, Liu, Qingyian, Nishimura, Nobuko, Peterkin, Tanya A.N., Yang, Kevin, Zhu, Jiawang, Riahi, Babak Bobby, Hungate, Randall W., Andersen, Neil G., Colyer, John T., Faul, Margaret M., Kamassah, Augustus, Wang, Judy, Jona, Janan, Kumar, Gondi, Johnson, Eileen, Askew, Benny C.
Published in Bioorganic & medicinal chemistry letters (01.06.2011)
Published in Bioorganic & medicinal chemistry letters (01.06.2011)
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An Efficient and Scalable One-Pot Double Michael Addition-Dieckmann Condensation for the Synthesis of 4,4-Disubstituted Cyclohexane β-Keto Esters
DeGraffenreid, Michael R, Bennett, Sarah, Caille, Sebastien, Gonzalez-Lopez de Turiso, Felix, Hungate, Randall W, Julian, Lisa D, Kaizerman, Jacob A, McMinn, Dustin L, Rew, Yosup, Sun, Daqing, Yan, Xuelei, Powers, Jay P
Published in Journal of organic chemistry (14.09.2007)
Published in Journal of organic chemistry (14.09.2007)
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Journal Article
Azole-based inhibitors of AKT/PKB for the treatment of cancer
Zeng, Qingping, Allen, John G., Bourbeau, Matthew P., Wang, Xianghong, Yao, Guomin, Tadesse, Seifu, Rider, James T., Yuan, Chester C., Hong, Fang-Tsao, Lee, Matthew R., Zhang, Shiwen, Lofgren, Julie A., Freeman, Daniel J., Yang, Suijin, Li, Chun, Tominey, Elizabeth, Huang, Xin, Hoffman, Douglas, Yamane, Harvey K., Fotsch, Christopher, Dominguez, Celia, Hungate, Randall, Zhang, Xiaoling
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
Published in Bioorganic & medicinal chemistry letters (01.03.2010)
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Journal Article
Aryl sulfones as novel Bradykinin B1 receptor antagonists for treatment of chronic pain
Biswas, Kaustav, Aya, Toshihiro, Qian, Wenyuan, Peterkin, Tanya A.N., Chen, Jian Jeffrey, Human, Jason, Hungate, Randall W., Kumar, Gondi, Arik, Leyla, Lester-Zeiner, Dianna, Biddlecome, Gloria, Manning, Barton H., Sun, Hong, Dong, Hong, Huang, Ming, Loeloff, Richard, Johnson, Eileen J., Askew, Benny C.
Published in Bioorganic & medicinal chemistry (01.09.2008)
Published in Bioorganic & medicinal chemistry (01.09.2008)
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